Borchard U
Institut für Pharmakologie, Heinrich-Heine-Universität Düsseldorf, Germany.
J Cardiovasc Pharmacol. 1994;24 Suppl 2:S85-91.
A great number of calcium antagonists are available for the treatment of cardiovascular diseases. Differences in pharmacodynamic and/or pharmacokinetic properties can be used to optimize therapy in patients and to minimize side effects. In contrast to all dihydropyridine (DHP) derivatives, drugs of the verapamil type slow atrioventricular conduction and are widely used for treatment of supraventricular tachycardia. The higher vasoselectivity of new DHP derivatives as compared with nifedipine should be regarded as an advantage for the treatment of patients with impaired left ventricular function. Besides vasodilation, additional effects such as antiatherosclerotic action, amelioration of rheological parameters, bronchial relaxation, or improvement of cerebral capacity in patients with cerebro-organic disorders have been documented for individual drugs. The long plasma half-life of some new calcium antagonists is advantageous with respect to patient compliance. Furthermore, a delayed increase in plasma concentration (high tmax values) is useful to minimize side effects such as reflex tachycardia, flush, headache, and dizziness.
有大量的钙拮抗剂可用于治疗心血管疾病。药效学和/或药代动力学特性的差异可用于优化患者的治疗并将副作用降至最低。与所有二氢吡啶(DHP)衍生物不同,维拉帕米类药物会减慢房室传导,广泛用于治疗室上性心动过速。与硝苯地平相比,新型DHP衍生物具有更高的血管选择性,这应被视为治疗左心室功能受损患者的一个优势。除血管舒张作用外,个别药物还具有抗动脉粥样硬化作用、改善流变学参数、支气管舒张或改善脑器质性疾病患者的脑功能等附加作用。一些新型钙拮抗剂的血浆半衰期较长,这对患者的依从性有利。此外,血浆浓度延迟升高(高tmax值)有助于将反射性心动过速、潮红、头痛和头晕等副作用降至最低。